CL 218872 

CL 218872 is an orally active and selective ligand for the benzodiazepine receptor subtype BZ₁. CL 218872 exhibits anxiolytic, sedative and anticonvulsant activities. CL 218872 can be used in researches of anxiety related disorders and epilepsy^{[1][2][3][4][5]}.

CL 218872 (ED₅₀ of 58 mg/kg; p.o.) inhibits footshock-induced fighting in mice with 50-fold lower potency than Diazepam^[2].
CL 218872 (5-20 mg/kg; p.o.) reduces locomotor activity, head-dipping, and rearing in rats, with sedative effects reversed by Flumazenil (HY-B0009)^[3].
CL 218872 (20-40 mg/kg; s.c.) antagonizes Diazepam-induced loss of righting reflex in mice^[4].
CL 218872 (5-20 mg/kg; i.p.) impairs place learning in rats, increasing swim path length and reducing quadrant bias in probe trials^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

278.24

C₁₃H₉F₃N₄

66548-69-4

Solid

Light yellow to brown

FC(C1=CC(C2=NN3C(C=C2)=NN=C3C)=CC=C1)(F)F

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Squires RF, et al. Some properties of brain specific benzodiazepine receptors: new evidence for multiple receptors. Pharmacol Biochem Behav. 1979 May;10(5):825-30.  [Content Brief]

  [2]. Oakley NR, et al. The benzodiazepine receptor ligand CL218,872 has both anxiolytic and sedative properties in rodents. Neuropharmacology. 1984 Jul;23(7A):797-802.  [Content Brief]

  [3]. File SE, et al. The sedative effects of CL 218,872, like those of chlordiazepoxide, are reversed by benzodiazepine antagonists. Psychopharmacology (Berl). 1985;85(3):295-300.  [Content Brief]

  [4]. Gee KW, et al. CL 218872 antagonism of diazepam induced loss of righting reflex: evidence for partial agonistic activity at the benzodiazepine receptor. Life Sci. 1983 Feb 28;32(9):1037-40.  [Content Brief]

  [5]. McNamara RK, et al. Like diazepam, CL 218,872, a selective ligand for the benzodiazepine omega 1 receptor subtype, impairs place learning in the Morris water maze. Psychopharmacology (Berl). 1992;107(2-3):347-51.  [Content Brief]